EP 1900731 A1 20080319 - N-(1-Phthalazin-1-yl-piperidin-4-yl)-amides as EP2-receptor modulators
Title (en)
N-(1-Phthalazin-1-yl-piperidin-4-yl)-amides as EP2-receptor modulators
Title (de)
N-(1-Phthalazin-1-yl-piperidin-4-yl)-amide als EP2-Rezeptor Modulatoren
Title (fr)
N-(1-Phthalazin-1-yl-piperidin-4-yl)-amides comme modulateurs du récepteur EP2
Publication
Application
Priority
EP 06090159 A 20060907
Abstract (en)
N-(1-Phthalazin-1-ylpiperidin-4-yl)amides, and its isomers, salts, and cyclodextrin clathrates are new. N-(1-Phthalazin-1-ylpiperidin-4-yl)amides of formula (I), and its isomers, salts, and cyclodextrin clathrates are new. W 1H, or 1-4C alkyl; X 1(CH 2) n, 2-4C alkenyl, or 2-4C alkynyl; n : 0-4; R 15-12-membered mono- or bicyclic aryl or heteroaryl ring, 5-12-membered mono- or bicyclic O-aryl or O-heteroaryl ring, S-aryl or S-heteroaryl ring, N-aryl or N-heteroaryl ring (all optionally mono- to trisubstituted), 1-6C alkyl, 3-10C cycloalkyl or 8-12-membered fused (hetero)arylcycloalkyl radical (all optionally substituted); R 2-R 51-6C alkyl, 3-10C cycloalkyl ring, 2-6C alkenyl, or 5-12-membered mono- or bicyclic aryl, heteroaryl ring (all optionally substituted), H, halogen, cyano, or OR 6, OC(O)R 6, S(O) n1R 6, SO 2NHR 6, SO 2NHC(O)R 6, NR 6R 7, NHC(O)R 6, CH 2NR 6R 7, CH 2NHC(O)R 6, C(OH)R 6R 7, C(O)R 6, CO 2R 6, or C(O)NR 6R 7; n 10-2; R 6and R 71-6C alkyl, 3-10C cycloalkyl ring, 5-12-membered mono- or bicyclic heteroaryl ring (all optionally substituted), H or 5-12-membered mono- or bicyclic aryl or heteroaryl ring; and R 6+R 73-8-membered ring. [Image] ACTIVITY : Antiinfertility; Gynecological; Cytostatic; Analgesic; Antimicrobial; Virucide; Antiinflammatory; Hepatotropic; Anti-HIV; Cardiovascular-Gen.; Vasotropic; Ophthalmological; CNS-Gen.; Respiratory-Gen.; Antiangiogenic; Neuroprotective; Nootropic; Immunomodulator; Nephrotropic. MECHANISM OF ACTION : Prostaglandin (EP 2) receptor modulator; EP 2receptor agonist; EP 2receptor antagonist. Compound -N-[1-(6-bromo-phthalazin-1-yl)-piperidin-4-yl]-2,3-dichloro-benzamide (Ia) was tested for EP 2receptor antagonist activity using cAMP antagonism assay. The compound (Ia) showed IC 50of 0.2 mu m.
Abstract (de)
Die vorliegende Erfindung betrifft Phthalazin-1-yl-piperidin-4-yl-amide der allgemeinen Formel i, Verfahren zu ihrer Herstellung sowie deren Verwendung zur Herstellung von pharmazeutischen Mitteln zur Behandlung von Erkrankungen und Indikationen, die im Zusammenhang stehen mit dem EP 2 Rezeptor.
IPC 8 full level
C07D 401/04 (2006.01); A61K 31/502 (2006.01); A61P 15/00 (2006.01)
CPC (source: EP US)
A61P 15/00 (2017.12 - EP); A61P 15/08 (2017.12 - EP); A61P 15/18 (2017.12 - EP); A61P 19/10 (2017.12 - EP); A61P 35/00 (2017.12 - EP); C07D 401/04 (2013.01 - EP US)
Citation (search report)
- [X] DE 2824064 A1 19781214 - PFIZER
- [DA] WO 03030911 A1 20030417 - MEDICAL RES COUNCIL [GB]
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA HR MK YU
DOCDB simple family (publication)
EP 1900731 A1 20080319; AR 062695 A1 20081126; CL 2007002578 A1 20080704; TW 200817356 A 20080416; US 2008146576 A1 20080619; UY 30572 A1 20080502; WO 2008028689 A1 20080313
DOCDB simple family (application)
EP 06090159 A 20060907; AR P070103952 A 20070907; CL 2007002578 A 20070905; EP 2007008081 W 20070906; TW 96132921 A 20070904; US 89692307 A 20070906; UY 30572 A 20070905